Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines

Hong Yu Li, Yan Wang, Lei Yan, Robert M. Campbell, Bryan D. Anderson, Jill R. Wagner, Jonathan M. Yingling

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

A novel series of 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines was synthesized and their TβR-1 inhibitory, p38 MAPK inhibitory, and TβR-1-dependent cellular activity were evaluated. Compound 5a was found to be a highly potent in the enzyme assay and TβR-1-dependent cellular assays. In addition, dimer (4g), with a urea linker, shows a similar enzyme and cellular activity despite a bulky substitution.

Original languageEnglish (US)
Pages (from-to)3585-3588
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number13
DOIs
StatePublished - Jul 5 2004
Externally publishedYes

Fingerprint

Quinolines
Enzyme Assays
p38 Mitogen-Activated Protein Kinases
Urea
Assays
Phosphotransferases
Enzymes
Dimers
Substitution reactions
TGF-beta type I receptor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor : 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines. / Li, Hong Yu; Wang, Yan; Yan, Lei; Campbell, Robert M.; Anderson, Bryan D.; Wagner, Jill R.; Yingling, Jonathan M.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 13, 05.07.2004, p. 3585-3588.

Research output: Contribution to journalArticle

Li, Hong Yu ; Wang, Yan ; Yan, Lei ; Campbell, Robert M. ; Anderson, Bryan D. ; Wagner, Jill R. ; Yingling, Jonathan M. / Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor : 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines. In: Bioorganic and Medicinal Chemistry Letters. 2004 ; Vol. 14, No. 13. pp. 3585-3588.
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